Results 21 to 30 of about 766,676 (298)

Licraside as novel potent FXR agonist for relieving cholestasis: structure-based drug discovery and biological evaluation studies

open access: yesFrontiers in Pharmacology, 2023
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi   +5 more
doaj   +1 more source

A–C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions [PDF]

open access: yes, 2018
Estrogen receptor-beta (ERβ) is a drug target for memory consolidation in postmenopausal women. Herein is reported a series of potent and selective ERβ agonists (SERBAs) with in vivo efficacy that are A–C estrogens, lacking the B and D estrogen rings ...
Donaldson, William A.   +12 more
core   +4 more sources

Immune Checkpoints as Therapeutic Targets in Autoimmunity

open access: yesFrontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch   +9 more
doaj   +1 more source

Reconciling intrinsic properties of activating TNF receptors by native ligands versus synthetic agonists

open access: yesFrontiers in Immunology, 2023
The extracellular domain of tumor necrosis factor receptors (TNFR) generally require assembly into a homotrimeric quaternary structure as a prerequisite for initiation of signaling via the cytoplasmic domains.
George Fromm   +2 more
doaj   +1 more source

Down Regulation with Luteal GnRH Agonist Therapy in Euploid Embryo Transfers Does Not Impact Pregnancy Rates [PDF]

open access: yes, 2020
Introduction : Gonadotropin-releasing hormone (GnRH) agonists have been used during assisted reproductive technology (ART) treatment for pituitary suppression and stimulation.
Bergin, MD, Keri   +4 more
core   +1 more source

Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]

open access: yes, 2015
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David   +17 more
core   +1 more source

In Vitro and In Silico Characterization of G-Protein Coupled Receptor (GPCR) Targets of Phlorofucofuroeckol-A and Dieckol

open access: yesMarine Drugs, 2021
Phlorotannins are polyphenolic compounds in marine alga, especially the brown algae. Among numerous phlorotannins, dieckol and phlorofucofuroeckol-A (PFF-A) are the major ones and despite a wider biological activity profile, knowledge of the G protein ...
Pradeep Paudel   +5 more
doaj   +1 more source

Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model

open access: yesMolecules, 2014
α1-Adrenoceptors (ARs; 1A, 1B, and 1D) have been determined to perform different prominent functions in the physiological responses of the sympathetic nervous system.
Fang Xu   +7 more
doaj   +1 more source

ALIX binds a YPX(3)L motif of the GPCR PAR1 and mediates ubiquitin-independent ESCRT-III/MVB sorting. [PDF]

open access: yes, 2012
The sorting of signaling receptors to lysosomes is an essential regulatory process in mammalian cells. During degradation, receptors are modified with ubiquitin and sorted by endosomal sorting complex required for transport (ESCRT)-0, -I, -II, and -III ...
Chen, Buxin   +7 more
core   +3 more sources

An Enantiomer of an Oral Small Molecule TSH Receptor Agonist Exhibits Improved Pharmacologic Properties

open access: yesFrontiers in Endocrinology, 2016
We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer.
Susanne Neumann   +7 more
doaj   +1 more source

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